Pharmacology of Serotonin Receptors and Ergot Alkaloids
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Questions and Answers

What type of receptor is negatively coupled to adenylyl cyclase and primarily acts in the Raphe Nucleus?

  • 5-HT 2A
  • 5-HT 1A (correct)
  • 5-HT 1B
  • 5-HT 2C

Which of the following antagonists is associated with the 5-HT 2A receptor?

  • Isamaltone
  • Ketanserin (correct)
  • 5-CAT
  • Spiperone (correct)

Which sub-type of the 5-HT receptor is primarily expressed in the stomach and fundus?

  • 5-HT 1D
  • 5-HT 2B
  • 5-HT 1B
  • 5-HT 2C (correct)

What effect is primarily mediated by the 5-HT 1D receptor?

<p>Inhibiting adenylyl cyclase (C)</p> Signup and view all the answers

What is the primary role of 5-HT3R antagonists?

<p>Act as anti-emetics (C)</p> Signup and view all the answers

What are the primary classifications of migraine according to clinical features?

<p>Migraine with aura (A), Migraine without aura (D)</p> Signup and view all the answers

What role do serotonin receptors 5-HT1B/D play during a migraine attack?

<p>Inhibit vasodilation (A)</p> Signup and view all the answers

What triggers can induce migraine episodes?

<p>Foods, drinks, and environmental cues (B)</p> Signup and view all the answers

Which of the following neuropeptides is released upon stimulation of trigeminal nerves during a migraine?

<p>Substance P (B)</p> Signup and view all the answers

What type of receptor is the 5-HT3 receptor classified as?

<p>Ligand-gated ion channel (A)</p> Signup and view all the answers

What characterizes ocular or retinal migraine?

<p>Temporary blindness and blurred vision (B)</p> Signup and view all the answers

Which of the following is positively coupled to adenylyl cyclase?

<p>5-HT4 receptor (C), 5-HT6 receptor (D)</p> Signup and view all the answers

Which region in the body is associated with the 5-HT4 receptor?

<p>Ileum (C)</p> Signup and view all the answers

What is the prototypical triptan drug used for migraine relief?

<p>Sumatriptan (A)</p> Signup and view all the answers

What is a known effect of the 5-HT7 receptor?

<p>Relaxation of smooth muscle (C)</p> Signup and view all the answers

Which mechanism is primarily involved in the maintenance of migraine pain?

<p>Decreased inhibition of central pain transmission (C)</p> Signup and view all the answers

What effect do triptans have when used during a migraine attack?

<p>Cause vasoconstriction (B)</p> Signup and view all the answers

Which of the following substances acts on the 5-HT6 receptor?

<p>Clozapine (B)</p> Signup and view all the answers

Which receptor is associated with the action of Lisuride?

<p>5-HT5 receptor (C)</p> Signup and view all the answers

What is the role of metergoline in serotonin pharmacology?

<p>Serotonin receptor antagonist (B)</p> Signup and view all the answers

In which regions is the 5-HT6 receptor primarily distributed?

<p>Thalamus and nucleus accumbens (C)</p> Signup and view all the answers

What is the primary distinction made between memorization and knowledge?

<p>Knowledge involves understanding relationships between concepts. (C)</p> Signup and view all the answers

Which resource is recommended for literature searches?

<p>South College Online Library (A)</p> Signup and view all the answers

What action is suggested if a concept does not make sense?

<p>Contact the Faculty who taught that concept. (D)</p> Signup and view all the answers

What is the recommended first step before scheduling an appointment with Faculty?

<p>Contact them via email to arrange a time. (A)</p> Signup and view all the answers

Which of the following is NOT listed as a resource for pharmacological studies?

<p>Social media platforms (D)</p> Signup and view all the answers

Which class of agents is primarily used as 5-HT1 agonists for migraine treatment?

<p>Triptans (C)</p> Signup and view all the answers

What is the primary mechanism of action (MOA) for serotonin agonists used in migraine therapy?

<p>Agonism of serotonin receptors (A)</p> Signup and view all the answers

What is the consequence of relying solely on memorization according to the content?

<p>It may only provide short-term assistance. (D)</p> Signup and view all the answers

Which textbook is explicitly required for coursework?

<p>Basic &amp; Clinical Pharmacology by Katzung. (A)</p> Signup and view all the answers

Which of the following conditions is treated using 5-HT4 agonists?

<p>Irritable bowel syndrome (C)</p> Signup and view all the answers

What adverse effect is commonly associated with the use of SSRIs?

<p>Serotonin syndrome (A)</p> Signup and view all the answers

What should students do if they have persistent concerns about course material?

<p>Contact Faculty for assistance. (C)</p> Signup and view all the answers

Which pharmacological class includes agents that are primarily 5-HT3 antagonists?

<p>Anti-emetics (C)</p> Signup and view all the answers

Which of the following is an example of a potential drug-drug interaction (DDI) that could lead to serotonin syndrome?

<p>MAOIs with SSRIs (C)</p> Signup and view all the answers

Which of the following pharmacokinetic aspects is crucial when considering the use of serotonergic agents?

<p>Half-life and metabolism (C)</p> Signup and view all the answers

What is a key characteristic of ergot alkaloids in the context of migraine treatment?

<p>They directly activate 5-HT1 receptors. (A)</p> Signup and view all the answers

What physiological functions are primarily regulated by 5-HT2A receptors?

<p>Cardiovascular function and muscle contraction (D)</p> Signup and view all the answers

Which drug functions as both a 5-HT2A receptor antagonist and an α1/α2 irreversible blocker?

<p>Phenoxybenzamine (B)</p> Signup and view all the answers

What is the primary indication for Ondansetron?

<p>Nausea and vomiting associated with surgery and chemotherapy (D)</p> Signup and view all the answers

Which of the following is a boxed warning for Alosetron?

<p>Increased risk of ischemic colitis (C)</p> Signup and view all the answers

What action does Tegaserod primarily facilitate in the gastrointestinal system?

<p>Facilitating acetylcholine release for peristalsis (A)</p> Signup and view all the answers

Which receptor type do 5-HT3 receptors represent?

<p>Ion channel (B)</p> Signup and view all the answers

Which of the following drugs is recognized for having anti-cholinergic activity along with being a 5-HT2A antagonist?

<p>Cyproheptadine (A)</p> Signup and view all the answers

What distinct risk is associated with potent 5-HT4 receptor agonists?

<p>Cardiac adverse effects (D)</p> Signup and view all the answers

Flashcards

5-HT 3 Receptor

A type of serotonin receptor that acts as a ligand-gated cation channel, meaning it opens when serotonin binds to it.

Serotonin Syndrome

A condition caused by excessive serotonin activity in the body, often due to interactions between medications.

Migraine

A type of headache characterized by intense, throbbing pain, often on one side of the head.

5-HT3 Antagonists

A group of drugs that work by blocking serotonin receptors, particularly in the gut.

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Selective Serotonin Reuptake Inhibitors (SSRIs)

Medications that increase serotonin levels in the brain, commonly used to treat depression.

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5-HT1 Agonists

Drugs that work by activating specific serotonin receptors, used in the treatment of migraines.

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5-HT4 Agonists

A class of drugs that target serotonin receptors to treat gastrointestinal conditions like Irritable Bowel Syndrome (IBS).

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Ergot Alkaloids

A group of drugs derived from ergot fungus, used to treat migraines.

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Pharmacokinetics (PK)

The process by which a drug is absorbed, distributed, metabolized, and eliminated from the body.

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5-HT3R antagonists: Anti-emetics

A type of serotonin receptor (5-HT3R) located in the area postrema of the brain, which is responsible for controlling nausea and vomiting. Antagonists of this receptor (5-HT3R antagonists), like ondansetron, block the action of serotonin at this receptor and act as anti-emetics

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Migraine without aura

A classification of migraine that occurs without any warning signs or sensory disturbances before the headache starts.

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Migraine with aura

A classification of migraine that involves sensory disturbances, like visual changes or tingling sensations, before the headache begins.

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Ocular or Retinal Migraine

A type of migraine that affects the eye or retina, causing blurred vision or temporary blindness.

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Migraine Triggers

Factors that can trigger a migraine attack, such as specific foods, drinks, chemicals, smells, emotional stress, or environmental changes.

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Calcitonin Gene-Related Peptide (CGRP)

A chemical found in the trigeminal nerve fibers, responsible for pain signaling during migraine attacks.

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5-HT1B/1D Receptors

A type of serotonin receptor that plays a significant role in migraine, controlling the release of CGRP and vasoconstriction.

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Triptans

A class of drugs that specifically target 5-HT1B/1D receptors, reducing CGRP release and constricting blood vessels, thereby relieving migraine attacks.

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5-HT2A Receptor Antagonists

Drugs that block the activity of 5-HT2A receptors. They are used to treat conditions related to serotonin overactivity.

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5-HT3 Receptor Antagonists

Drugs that block the activity of 5-HT3 receptors. They are commonly used to treat nausea and vomiting.

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5-HT4 Receptor Agonist

Drugs that activate 5-HT4 receptors. They are used to treat disorders of the gastrointestinal tract.

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Nausea and Vomiting (N/V)

A common side effect of medications that interact with the serotonin system. It is characterized by nausea and vomiting.

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Understanding Concepts vs. Memorization

Understanding concepts goes beyond simply memorizing facts. It involves actively thinking about the relationships between different ideas, leading to a deeper, more meaningful comprehension.

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Seeking Help When Concepts Are Unclear

If a concept doesn't make sense, thoroughly research it using available resources such as textbooks, online databases, or online resources. Don't be afraid to ask for help from faculty members.

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Contacting Faculty for Clarification

Contacting faculty members via email is recommended for scheduling an appointment to discuss challenging concepts. This allows the faculty member to allocate sufficient time to address your concerns thoroughly.

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Canvas iMCP3: A Valuable Learning Resource

Canvas iMCP3 is an online platform offering study resources and videos that can be utilized for effective learning.

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South College Library: A Treasure Trove of Resources

The South College Library provides online access to various resources, including guidelines, databases like AccessPharmacy, Micromedex, Lexicomp, and literature search tools like PubMed and Discover search.

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Goodman & Gilman: A Cornerstone Textbook

Goodman & Gilman's The Pharmacological Basis of Therapeutics is a comprehensive textbook that provides a foundation in the mechanisms of drug action and their clinical applications.

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Foye's Principles of Medicinal Chemistry: Chemical Foundations of Pharmacology

Foye's Principles of Medicinal Chemistry, 15th Edition, serves as a reference text that covers the chemical principles underlying drug action, synthesis, and development.

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Pharmacogenomics: Understanding Drug Responses based on Genetics

Pharmacogenomics: An Introduction and Clinical Perspective by Joseph S. Bertino Jr. et al. offers insights into the study of how genetic variations influence drug responses.

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Study Notes

Pharmacology of Serotonin Receptor Agonists and Antagonists, and Ergot Alkaloids

  • Maha Abdalla, PharmD, PhD, RPh is an Associate Professor of Pharmaceutical Sciences at South College.
  • Office Room: 276
  • Phone: (865)288-5837
  • Office Hours: Tuesday & Thursday 9 am - 12 pm or by appointment.
  • Email: [email protected]

Serotonin (5-hydroxytryptamine, aka 5-HT)

  • Bio synthesis & Metabolism
  • Serotonin Receptors: GPCR: 5-HT₁R, 5-HT₂R, 5-HT₄R. Na/K ion channel: 5-HT₃R
  • Migraine Management (Headache Society Consensus Statement): Update on integrating new migraine treatments into clinical practice.

Triptans

  • Selective 5-HT₁B/D type receptor agonist
  • Sumatriptan, rizatriptan, zolmitriptan, eletriptan, almotriptan, naratriptan, frovatriptan

Ergot Alkaloids

  • Nonselective 5-HT agonist
  • Dihydroergotamine (Migranal), Ergotamine (Ergomar)
  • CGRP Receptor Antagonist:
  • BOTH prophylaxis & acute treatment: Nurtec ODT (rimegepant) – PO
  • Ubrelvy (ubrogepant)-PO, Zavzpret (zavegepant)- Nasal spray
  • Qulipta (atogepant) – PO
  • Aimovig (erenumab-aooe)-subQ
  • Emgality (galcanezumab-gnlm), Ajovy (fremanezumab-vfrm)
  • Vyepti (Eptinezumab-jjmr)

5-HT2 Receptor Antagonist

  • Antidepressant and Antipsychotics: Olanzapine, clozapine, Risperidone

5-HT3 Receptor Antagonist

  • Antiemetic: Ondansetron
  • Alosetron - Restricted Use

5-HT4 receptors partial agonists

Serotonin Syndrome

  • Other drug classes that affect serotonin levels:
    • Selective Serotonin Reuptake Inhibitors (SSRIs): Sertraline, fluoxetine, paroxetine, citalopram, escitalopram
    • Monoamine Oxidase Inhibitors (MAOIs): Tranylcypromine, phenelzine

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Description

This quiz covers the pharmacology of serotonin receptor agonists and antagonists, focusing specifically on their biosynthesis, metabolism, and role in migraine management. It also includes key information about triptans and ergot alkaloids, along with the pharmacological implications of CGRP receptor antagonists in treatment. Test your knowledge on these essential topics in pharmaceutical sciences.

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